专利号:US-5322852-A 优先权日:1992-02-17 标 题:Aminooxy piperidines as ornithine decarboxylase inhibitors 发明人:FREI JOERG; STANEK JAROSLAV 权利人:CIBA GEIGY CORP 摘要:The invention relates to compounds of formula I (I) wherein either R1 is a radical of formula Ia, -(CH2)n-O-NH2(Ia) in which n is 0 or 1, is hydrogen and R2 is a radical of formula Ib, -(CH2)p-O-NH2(Ib) in which p is 1 or 2, and wherein R is C1-C2alkyl which is attached to one carbon atom of the central piperidine ring system, but not to the same carbon atom as R1 of formula Ia or as R2 of formula Ib; and m is 1 or 2, and salts thereof. The invention further relates to the preparation of these compounds, to intermediates obtained during their synthesis, to pharmaceutical compositions which contain them, and to the use of said compounds for the therapeutic treatment of the human or animal body and for the preparation of pharmaceutical compositions. The compounds of formula I are inhibitors of ornithin decarboxylase.
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[参考文献]: Karen A Nolan, Et Al. In Silico Identification And Biochemical Characterization Of Novel Inhibitors Of Nqo1. Bioorg Med Chem Lett. 2006 Dec 15;16(24):6246-54.
合成参考文献
摘要:Singh, F. V., Science of Synthesis Knowledge Updates, (2021) 1, 208. 摘要:Singh, F. V., Science of Synthesis Knowledge Updates, (2021) 1, 210.